High Throughput Screening: Methods and Protocols

1. Design and Implementation of High Throughput Screening Assays
David J. Powell, Robert P. Hertsberg,and Ricardo Macarr n

2. Characterization of InhibitorBinding Through Multiple Inhibitor Analysis: A Novel Local Fitting Method
Thomas V. Riera, Tim J. Wigle, andRobert A. Copeland

3. High Throughput Screening UsingMass Spectrometry within Drug Discovery
Mattias Rohman and Jonathan Wingfield

4. Structure-Based Virtual Screeningof Commercially Available Compound Libraries
Dmitri Kireev

5. AlphaScreen-Based Assays:Ultra-High Throughput Screening for Small Molecule Inhibitors of ChallengingEnzymes and Protein-Protein Interactions
Adam Yasgar, Ajit Jadhav, AntonSimeonov, and Nathan P. Coussens

6. Instrument Quality Control
Chatura Jayakody and Emily A.Hull-Ryde

7. Application of FluorescencePolarization in HTS Assays<Xinyi Huang and Ann Aulabaugh

8. Time Resolved Fluorescence Assays
Chen-Ting Ma and Eduard A. Sergienko

9. Protein Kinase SelectivityProfiling Using Microfluid Mobility Shift Assays
Peter Drueckes

10. Screening for Inhibitors ofKinase Autophosphorylation
Bianca Heedmann and Martin Klumpp

11. A Fluorescence-Based HighThroughput Screening Assay to Identify Growth Inhibitors of the PathogenicFungus Aspergillus fumigatus
Thomas M. Smith, Daryl L. Richie,Jianshi Tao

12. Mycobacterium tuberculosisHigh Throughput Screening
E. Lucile White, Nichole A. Tower,and Lynn Rasmussen

13. Identification ofState-Dependent Blockers for Voltage Gated Calcium Channels Using a FLIPR BasedAssay
Alberto di Silvio

14. A Luciferase Reporter GeneSystem for High Throughput Screening of Gamma-Globin GeneActivators
Wensheng Xie, Robert Silvers, MichaelOuellette, Zining Wu, Quinn Lu, Hu Li, Kathleen Gallagher, Kathy Johnson, andMonica Montoute

15. A High Throughput Flow CytometryAssay for Identification of Inhibitors of 3', 5'-Cyclic Adenosine MonophosphateEfflux
Dominique Perez, Peter C. Simons,Yelena Smagley, Larry A. Sklar, and Alexandre Chigaev

16. High Throughput Cell ToxicityAssays
David Murray, Lisa McWilliams, andMark Wigglesworth

17. BRETⁿ: NanoLuc-BasedBioluminescence Resonance Energy Transfer Platform to Monitor Protein-ProteinInteractions in Live Cells
Xiu-Lei Mo and Haian Fu

18. Application of Imaging-BasedAssays in Microplate Formats for High Content Screening
Adam I. Fogel, Scott E. Martin, andSamuel A. Hasson